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抗菌细菌胺碳酸:从设计到体内活性

Daria Elżbieta Nawrot¹, Ghada Bouz¹, Ondřej Janďourek¹

¹Faculty of Pharmacy in Hradec Králové, Charles University, Heyrovského 1203, 50005, Hradec Králové, Czech Republic.

European journal of medicinal chemistry

|July 9, 2023

概括

一种新型化合物通过抑制甲氨酸代谢,有效向对药物敏感和耐药的结核病菌株. 与现有治疗方法相比,这种有前途的抗结核药物没有毒性,并且具有更好的代谢稳定性.

科学领域:

药用化学医学化学
微生物学微生物学
药物发现药物发现药物发现

背景情况:

结核病 (TB) 仍然是全球领先的传染病杀手.
新出现的抗菌素耐药性需要针对Mycobacterium tuberculosis (Mtb) 的新型治疗策略.

研究的目的:

合成和评估新型抗结核药物,有效对药物敏感和耐药的Mtb菌株.
为了识别比现有的结核病疗法更好的安全性和药理动力学特征的化合物.

主要方法:

新型化合物系列的合成,通过将异化,化和4 - 氨基酸的碎片结合起来.
在体外对MTB H37Rv菌株进行抗菌细菌活性测试.
在鼠类结核病模型中的体内疗效评估.
生物化学测定,in silico模拟和人类肝脏微小细胞中的代谢稳定性研究.

主要成果:

化合物10c在体外表现出强大,有选择性的活性,对药物敏感和耐药的Mtb.
在小鼠结核病模型中,化合物10c在体外或体内没有表现出细胞毒性,并在脏中减少了细菌负载.
生物化学研究表明,10c化合物向的是 metionin代谢,而不是叶酸途径.
在基分析表明,它与菌根菌的甲氨酸-tRNA合成酶结合.
化合物10c表现出良好的代谢稳定性 (630分半衰期) 和没有有毒代谢物.

结论:

化合物10c是一种有前途的新型抗结核候选物,具有独特的作用机制.
该化合物克服了异化和4 - 氨酸的关键限制,为改善结核病治疗提供了潜力.

关键词:

4 - 氨基酸4-氨基酸伊索尼亚齐德的使用方法多种药物耐药性多种药物耐药性皮拉津胺的使用方法氨酸是什么? 氨酸是什么?结核病是一种疾病.

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